Anticonvulsant evaluation and mechanism of action of benzylamino enaminones

Bioorganic & Medicinal Chemistry
Ivan O EdafioghoSamuel B Kombian

Abstract

The mechanism of anticonvulsant action was evaluated for the benzylamino enaminones. The most potent enaminone in this series was the unsubstituted benzylamine analog (30; methyl 4-benzylamino-6-methyl-2-oxocyclohex-3-en-1-oate) which had an oral effective dose (ED50) in rats of 27 mg/kg against maximal electroshock seizures, and a concentration 10-fold less than this dose depressed excitatory synaptic transmission, and action potential firing in the rat brain in vitro.

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Citations

Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Juean DengZongzhou Zhou
Nov 9, 2011·Acta Crystallographica. Section E, Structure Reports Online·Patrice L JacksonRay J Butcher
Dec 18, 2010·The Journal of Pharmacology and Experimental Therapeutics·Ze-Jun WangThomas Heinbockel
Jan 25, 2012·International Journal of Molecular Sciences·Juan C Garro MartinezEduardo A Castro
Feb 26, 2014·European Journal of Medicinal Chemistry·Ivan O EdafioghoSamuel B Kombian
Dec 20, 2014·Pharmaceuticals·Thomas HeinbockelPatrice L Jackson-Ayotunde
Dec 18, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Muhammad NisarMd Saiful Islam
Oct 10, 2014·Expert Opinion on Drug Discovery·Juan C Garro MartinezMario R Estrada
Jul 11, 2007·Journal of Pharmaceutical Sciences·Ivan O EdafioghoK R Scott
Jul 30, 2011·Life Sciences·Ahmed Z El-HashimSamuel B Kombian

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